Ирбесартан
Ирбесартан химические свойства, назначение, производство
Описание
Avapro was launched in Germany, the UK and the US for hypertension. It
can be prepared in six steps starting with cyclopentanone or in three steps from 1-
aminocyclopentanecarboxylic acid ethyl ester and pentanimidic ethyl ester. Avapro is
an angiotensin Ⅱ receptor antagonist that is non-competitive and selective for AT,
subtypes and has no AT2 activity at postsynaptic receptors compared to presynatpic. It
has no affinity for various non angiotensin Ⅱ receptor types in binding, no interaction
with calcium channels or antiports, and no affinity for α1- and α2--adrenoreceptors,
serotonergic receptors, muscarinic m1 and m2 or other receptors. It is as potent as
saralasin but with no agonist activity and is 10 times more potent than DuP753 in rats.
It is similar in efficacy to enalapril (in those with severe hypertension) and atenolol,
while more effective than losartan for mild to moderate hypertension.
Химические свойства
Crystalline Solid
Использование
For the treatment of hypertension, as well as diabetic nephropathy with an elevated serum creatinine and proteinuria (>300 mg/day) in patients with type 2 diabetes and hypertension. Irbesartan is also used as a second line agent in the treatment of conges
Определение
ChEBI: A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.
Общее описание
Irbesartan, 2-butyl-3-[[29-(1H-tetrazol-5-yl)[1,19-biphenyl]-4-yl]methyl]1,3-diazaspiro[4,4]non-1en-4-one (Avapro), like losartan, possesses the acidic tetrazolesystem, which most likely plays a role, similar to the acidicgroups of angiotensin II, in binding to the angiotensin II receptor.In addition, the biphenyl system that serves to separatethe tetrazole from the aliphatic nitrogen is still present.A major difference in this agent is that it does not possessthe acidic side chain. Even so, irbesartan has good affinityfor the angiotensin II receptor because of hydrogen bondingwith the carbonyl moiety of the amide system. Also, thisparticular agent does not require metabolic activation ascandesartan does.
Ирбесартан препаратная продукция и сырье
сырьё
препарат
Ирбесартан поставщик
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